Long-acting matrix tablet formulations

• US 4,704,284 A
• Filed: 08/12/1982
• Issued: 11/03/1987
• Est. Priority Date: 08/12/1982
• Status: Expired due to Term

• Current Assignee: Pfizer Inc.
• Original Assignee: Pfizer Inc.
• Inventors: Boettner, Wayne A., Beatty, Morgan L.
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/407,511
• Time in Patent Office: 1,909 Days
• Field of Search: 424/19-22, 424/35, 424/36, 424/38, 424/469
• US Class Current: 424/469
• CPC Class Codes: A61K 9/2004 Excipients; Inactive ingredients
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets

Abstract

A pharmaceutical tablet which releases an initial burst of therapeutic agent and thereafter releases the agent at an essentially constant rate comprising an acid soluble therapeutic agent in an insoluble matrix, the tablet containing an acid insoluble, base soluble pharmaceutically acceptable component selected from polymers and fatty acids, a pharmaceutically acceptable organic acid and at least one pharmaceutically acceptable excipient, the component and the acid each being present in an amount of from about 1-25 percent by weight of the total composition.

Claims

1. A pharmaceutical tablet which releases an initial burst of therapeutic agent and thereafter releases said agent at an essentially constant rate comprising an acid-soluble therapeutic agent, an acid-insoluble, base-soluble pharmaceutically acceptable polymeric acid phthalate, and a pharmaceutically acceptable polycarboxylic acid in an insoluble matrix consisting of ethyl cellulose, hydrogenated vegetable oil or mixtures thereof, said phthalate being present in an amount of from about 1 to 25 percent by weight of said tablet, said acid being present in an amount of from about 7 to 20% by weight of said tablet, said matrix components being present in an amount of from about 2-10% by weight of said tablet and said therapeutic agent being present in an amount of from about 25-75% by weight of said tablet.

2. The tablet of claim 1 wherein said phthalate is hydroxypropyl methylcellulose phthalate and said acid is citric acid.

3. The tablet of claim 2 wherein said phthalate is present in an amount of from 3-15 percent by weight.

4. The tablet of claim 1 wherein said therapeutic agent is trimazosin.

5. The tablet of claim 1 comprising about 40-60 weight % trimazosin, about 4-5 weight % ethyl cellulose, about 12-15 weight % citric acid and about 3-7 weight percent hydroxypropyl methylcellulose phthalate.

6. The tablet of claim 5 which also contains from about 7-8 weight percent zein.